1. GPCR/G Protein
  2. GCGR GLP Receptor
  3. Retatrutide acetate

Retatrutide (LY3437943) acetate is a triple agonist peptide of the glucagon receptor (GCGR), glucosedependent insulinotropic polypeptide receptor (GIPR), and glucagon-like peptide-1 receptor (GLP-1R). Retatrutide acetate inhibits human GCGR, GIPR, and GLP-1R with EC50 values of 5.79, 0.0643 and 0.775 nM, respectively. Retatrutide acetate can be used for the research of obesity.

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Top Publications Citing Use of Products
In Vivo Efficacy Study
Histological Imaging/Staining
IHC

    Retatrutide acetate purchased from MedChemExpress. Usage Cited in: NPJ Metab Health Dis. 2025;3(1):10.  [Abstract]

    Mice were subcutaneously administered either Veh, 30 nmol/kg Retatrutide, or 30 nmol/kg SEMA every other day before the initiation of the dark cycle at 5 pm. Survival curves were plotted as % of mice tumor-free for each group.

    Retatrutide acetate purchased from MedChemExpress. Usage Cited in: NPJ Metab Health Dis. 2025;3(1):10.  [Abstract]

    Mice were subcutaneously administered either Veh, 30 nmol/kg Retatrutide, or 30 nmol/kg SEMA every other day before the initiation of the dark cycle at 5 pm. Frequencies of CD45+ cells/live cells were shown.

    Retatrutide acetate purchased from MedChemExpress. Usage Cited in: Endocrine. 2025 Jan;87(1):159-169.  [Abstract]

    The mice received daily subcutaneous injections of 10 nmol/kg of Retatrutide for 10 weeks. Changes in fasting blood glucose (FBG) of mice in each group were recorded.

    Retatrutide acetate purchased from MedChemExpress. Usage Cited in: Endocrine. 2025 Jan;87(1):159-169.  [Abstract]

    The mice received daily subcutaneous injections of 10 nmol/kg of Retatrutide for 10 weeks. Representative HE and PAS stained images of the kidneys of mice in each group were obtained.

    Retatrutide acetate purchased from MedChemExpress. Usage Cited in: Endocrine. 2025 Jan;87(1):159-169.  [Abstract]

    The mice received daily subcutaneous injections of 10 nmol/kg of Retatrutide for 10 weeks. Representative immunohistochemical staining of TNF-α, Caspase-1, NLRP3, fibronectin, collagen I, and α-SMA in renal tissue of mice in each group was performed.
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    Description

    Retatrutide (LY3437943) acetate is a triple agonist peptide of the glucagon receptor (GCGR), glucosedependent insulinotropic polypeptide receptor (GIPR), and glucagon-like peptide-1 receptor (GLP-1R). Retatrutide acetate inhibits human GCGR, GIPR, and GLP-1R with EC50 values of 5.79, 0.0643 and 0.775 nM, respectively. Retatrutide acetate can be used for the research of obesity[1].

    IC50 & Target

    EC50 (for human): 5.79 (GCGR), 0.0643 (GIPR), 0.775 nM (GLP-1R) [1].
    EC50 (for mouse): 2.32 (GCGR), 0.191 (GIPR), 0.794 nM (GLP-1R) [1].
    Ki (for human): 5.6 (GCGR), 0.057 (GIPR), 7.2 nM (GLP-1R) [1].
    Ki (for mouse): 73 (GCGR), 2.8 (GIPR), 1.3 nM (GLP-1R)[1].

    In Vitro

    Retatrutide (LY3437943) acetate has efficacy for human GCGR, GIPR, and GLP-1R with EC50 values of 5.79, 0.0643 and 0.775 nM, respectively[1].
    Retatrutide acetate has efficacy for mouse GCGR, GIPR, and GLP-1R with EC50 values of 2.32, 0.191 and 0.794 nM, respectively[1].
    Retatrutide acetate has binding affinity for human GCGR, GIPR, and GLP-1R with Ki values of 5.6, 0.057 and 7.2 nM, respectively[1].
    Retatrutide acetate has binding affinity for mouse GCGR, GIPR, and GLP-1R with Ki values of 73, 2.8 and 1.3 nM, respectively[1].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    In Vivo

    Retatrutide (LY3437943) acetate (s.c.; 47 μg/kg; single) engages GCGR in vivo and can improve glucose tolerance in an ipGTT through either the GIP or GLP-1 receptors[1].
    Retatrutide acetate (s.c.; 10 mL/kg; cycle every 3 days; for 21 days) causes great body weight loss and increases energy expenditure through glucagon receptor activatio[1].
    Retatrutide acetate has safety and tolerability[1].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Clinical Trial
    Molecular Weight

    4731.33 (free base)

    Formula

    C221H342N46O68.xC2H4O2

    Sequence

    Tyr-{Aib}-Gln-Gly-Thr-Phe-Thr-Ser-Asp-Tyr-Ser-Ile-{a-Me-Leu}-Leu-Asp-Lys-Lys(AEEA-γGlu-C20 diacid)Ala-Gln-{Aib}-Ala-Phe-Ile-Glu-Tyr-Leu-Leu-Glu-Gly-Gly-Pro-Ser-Ser-Gly-Ala-Pro-Pro-Pro-Ser-NH2

    Sequence Shortening

    Y-{Aib}-QGTFTSDYSI-{α-Me-Leu}-LDK-Lys(AEEA-γGlu-C20 diacid)-AQ-{Aib}-AFIEYLLEGGPSSGAPPPS-NH2

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage

    Please store the product under the recommended conditions in the Certificate of Analysis.

    Purity & Documentation
    References
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    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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    Product Name:
    Retatrutide acetate
    Cat. No.:
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